For more than 60 years, N-thiolated β-lactam antibiotics have played an essential role in treating bacterial infections (Morin et al., 1982 and Kukacs et al., 1990). The development of multi-drug resistant Staphylococcus infections is an increasing concern for the global health community. Infection caused by methicillin-resistant Staphylococcus aureus (MRSA) is becoming increasingly difficult to treat with conventional antibiotics, leading to a sharp rise in clinical complications. Recently a new class of N-thiolated β-lactam has been found to inhibit bacterial growth in Staphylococcus aureus (Turos et al., 2000) including methicillin-resistant Staphylococcus aureus (MRSA) strains.